《Discovery of Potent and Selective Inhibitors of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Protein Kinase as Potential Anticancer Agents》 was written by Charrier, Jean-Damien; Durrant, Steven J.; Golec, Julian M. C.; Kay, David P.; Knegtel, Ronald M. A.; MacCormick, Somhairle; Mortimore, Michael; O’Donnell, Michael E.; Pinder, Joanne L.; Reaper, Philip M.; Rutherford, Alistair P.; Wang, Paul S. H.; Young, Stephen C.; Pollard, John R.. Application of 918439-76-6 And the article was included in Journal of Medicinal Chemistry on April 14 ,2011. The article conveys some information:
DNA-damaging agents are among the most frequently used anticancer drugs. However, they provide only modest benefit in most cancers. This may be attributed to a genome maintenance network, the DNA damage response (DDR), that recognizes and repairs damaged DNA. ATR is a major regulator of the DDR and an attractive anticancer target. Herein, we describe the discovery of a series of aminopyrazines with potent and selective ATR inhibition. Compound (I) inhibits ATR with a Ki of 6 nM, shows >600-fold selectivity over related kinases ATM or DNA-PK, and blocks ATR signaling in cells with an IC50 of 0.42 μM. Using I, here it is shown that ATR inhibition markedly enhances death induced by DNA-damaging agents in certain cancers but not normal cells. This differential response between cancer and normal cells highlights the great potential for ATR inhibition as a novel mechanism to dramatically increase the efficacy of many established drugs and ionizing radiation. In the experimental materials used by the author, we found (S)-3-Iodotetrahydrofuran(cas: 918439-76-6Application of 918439-76-6)
(S)-3-Iodotetrahydrofuran(cas: 918439-76-6) is one of organic iodides. The carbon-iodine bond is weaker than other carbon-halogen bonds due to the poor electronegative nature of the iodine atom. In general, organic iodides are light-sensitive and turn yellow during storage, owing to the formation of iodine. Organic iodides can be alkyl, alkenyl, or alkynyl, and all of them are very reactive toward with many kinds of nucleophiles.Application of 918439-76-6
Referemce:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem